AS2444697|cas:1287665-60-4|西域试剂

AS2444697,98.13%

产品编号：Bellancom-18992| CAS NO：1287665-60-4| 分子式：C₁₉H₂₁ClN₆O₄| 分子量：432.86

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18992	￥1300.00	杭州北京（现货）
Bellancom-18992	￥2100.00	杭州北京（现货）
Bellancom-18992	￥7200.00	杭州北京（现货）
Bellancom-18992	￥11500.00	杭州北京（现货）

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AS2444697

产品介绍

AS2444697 是一种具有口服活性的 IRAK-4 抑制剂，IC₅₀ 为 21 nM。 AS2444697 有效抑制人和大鼠 IRAK-4 活性。AS2444697 通过抗炎作用表现出肾脏保护作用。

生物活性

AS2444697 is an orally active IRAK-4 inhibitor with an IC₅₀ of 21 nM. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action.

体外研究

体内研究

AS2444697 is efficacious in the rat adjuvant-induced arthritis (ED₅₀ 2.7 mg/kg, BID, PO) and the rat collagen-induced arthritis (ED₅₀ 1.6 mg/kg, BID, PO) disease models. Good bioavailability was seen in rat (F% 50) and dog (F% 78) pharmacokinetic studies.
AS2444697 (0.3-3 mg/kg) significantly increases the plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) in LPS/GalN-treated mice. Single administration of AS2444697 (0.3-3 mg/kg) dose-dependently decreases plasma levels of these all parameters, and these effects were significant at doses of 1 mg/kg or higher.
After oral administration of AS2444697 (3 mg/kg) to 5/6 Nx rats, plasma, and tissue (liver and kidney) concentrations of the unchanged drug peaked at 1 h and then gradually decreased, with a terminal half-life of 2.7-2.9 h.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male 6-week-old Wistar rats and Balb/c mice
Dosage:	0.3-3 mg/kg
Administration:	Single administration; orally
Result:	The plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) were significantly increased.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male 6-week-old Wistar rats and Balb/c mice
Dosage:	0.3-3 mg/kg
Administration:	Single administration; orally
Result:	The plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) were significantly increased.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 12.5 mg/mL (28.88 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3102 mL	11.5511 mL	23.1022 mL
5 mM	0.4620 mL	2.3102 mL	4.6204 mL
10 mM	0.2310 mL	1.1551 mL	2.3102 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 1.67 mg/mL (3.86 mM); Suspended solution; Need ultrasonic

此方案可获得 1.67 mg/mL (3.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.67 mg/mL (3.86 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.86 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。